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EP0348911A3 - 19-fluoro- or cyano- 21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors - Google Patents

19-fluoro- or cyano- 21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors Download PDF

Info

Publication number
EP0348911A3
EP0348911A3 EP89111699A EP89111699A EP0348911A3 EP 0348911 A3 EP0348911 A3 EP 0348911A3 EP 89111699 A EP89111699 A EP 89111699A EP 89111699 A EP89111699 A EP 89111699A EP 0348911 A3 EP0348911 A3 EP 0348911A3
Authority
EP
European Patent Office
Prior art keywords
fluoro
cyano
hydroxylase inhibitors
derivatives useful
hydroxyprogesterone derivatives
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP89111699A
Other versions
EP0348911A2 (en
EP0348911B1 (en
Inventor
Gene W. Holbert
J. O'neal Johnston
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Aventis Pharmaceuticals Inc
Original Assignee
Merrell Dow Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merrell Dow Pharmaceuticals Inc filed Critical Merrell Dow Pharmaceuticals Inc
Priority to AT89111699T priority Critical patent/ATE100462T1/en
Publication of EP0348911A2 publication Critical patent/EP0348911A2/en
Publication of EP0348911A3 publication Critical patent/EP0348911A3/en
Application granted granted Critical
Publication of EP0348911B1 publication Critical patent/EP0348911B1/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
    • C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Toxicology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Manufacture Of Macromolecular Shaped Articles (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
  • Organic Insulating Materials (AREA)

Abstract

19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.
EP89111699A 1988-06-28 1989-06-27 19-fluoro- or cyano- 21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors Expired - Lifetime EP0348911B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AT89111699T ATE100462T1 (en) 1988-06-28 1989-06-27 19-FLUOROOR OR CYANO-21-HYDROXY-PROGESTERONE DERIVATIVES AS 19-HYDROXYLASE INHIBITORS.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/212,410 US4920114A (en) 1988-06-28 1988-06-28 19-fluoro- or cyano-21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors
US212410 2002-08-05

Publications (3)

Publication Number Publication Date
EP0348911A2 EP0348911A2 (en) 1990-01-03
EP0348911A3 true EP0348911A3 (en) 1990-03-28
EP0348911B1 EP0348911B1 (en) 1994-01-19

Family

ID=22790899

Family Applications (1)

Application Number Title Priority Date Filing Date
EP89111699A Expired - Lifetime EP0348911B1 (en) 1988-06-28 1989-06-27 19-fluoro- or cyano- 21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors

Country Status (19)

Country Link
US (1) US4920114A (en)
EP (1) EP0348911B1 (en)
JP (1) JP2727466B2 (en)
KR (1) KR0140885B1 (en)
CN (1) CN1039424A (en)
AT (1) ATE100462T1 (en)
AU (1) AU610413B2 (en)
CA (1) CA1321579C (en)
DE (1) DE68912422T2 (en)
DK (1) DK318489A (en)
ES (1) ES2061802T3 (en)
FI (1) FI893162A7 (en)
HU (1) HUT51289A (en)
IL (1) IL90728A0 (en)
NO (1) NO892679L (en)
NZ (1) NZ229694A (en)
PH (1) PH25771A (en)
PT (1) PT90989B (en)
ZA (1) ZA894753B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4433374A1 (en) * 1994-09-20 1996-03-21 Hoechst Ag 17-deoxi-corticosteroid-21- / O / -carboxylic acid ester, process for their preparation and medicaments containing them
US6787530B1 (en) 1996-08-23 2004-09-07 Monash University Use of pregnane-diones as analgesic agents

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3205228A (en) * 1963-03-01 1965-09-07 Syntex Corp 19-substituted pregnenes
EP0047016A1 (en) * 1980-09-02 1982-03-10 Merrell Dow Pharmaceuticals Inc. Progesterone derivatives, process for their production, and pharmaceutical compositions
EP0056000A2 (en) * 1979-07-31 1982-07-14 Roussel-Uclaf 17-(Alkoxycarbonyl)(formamide)methylene steroid derivatives and their preparation

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3124574A (en) * 1964-03-10 Iz-halo pregnenes
US3154569A (en) * 1961-10-10 1964-10-27 Vismara Francesco Spa 19-nitrilosteroids and process for producing 19-norsteroids
IT1051705B (en) * 1962-05-12 1981-05-20 Vismara Spa F METHOD FOR THE PREPARATION OF STEROID INTERMEDIATES
GB984093A (en) * 1962-02-19 1965-02-24 Syntex Corp Improvements in or relating to 19-halo-pregnane compounds
US3257435A (en) * 1962-09-21 1966-06-21 Syntex Corp 19-bisdifluoro pregnanes
US3257389A (en) * 1962-09-21 1966-06-21 Syntex Corp 19-bisdifluoro-pregnanes
US3159620A (en) * 1963-05-22 1964-12-01 Vismara Francesco Spa Process for the preparation of 17 alpha-ethynyl-19-norandrostene compounds
US3394128A (en) * 1964-09-26 1968-07-23 Syntex Corp 19-halo-androstane and pregnane derivatives and processes for the preparation thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3205228A (en) * 1963-03-01 1965-09-07 Syntex Corp 19-substituted pregnenes
EP0056000A2 (en) * 1979-07-31 1982-07-14 Roussel-Uclaf 17-(Alkoxycarbonyl)(formamide)methylene steroid derivatives and their preparation
EP0047016A1 (en) * 1980-09-02 1982-03-10 Merrell Dow Pharmaceuticals Inc. Progesterone derivatives, process for their production, and pharmaceutical compositions

Also Published As

Publication number Publication date
EP0348911A2 (en) 1990-01-03
DK318489A (en) 1989-12-29
IL90728A0 (en) 1990-01-18
HUT51289A (en) 1990-04-28
KR0140885B1 (en) 1998-06-15
CA1321579C (en) 1993-08-24
EP0348911B1 (en) 1994-01-19
DE68912422T2 (en) 1994-08-18
NZ229694A (en) 1992-03-26
US4920114A (en) 1990-04-24
FI893162L (en) 1989-12-29
FI893162A7 (en) 1989-12-29
ATE100462T1 (en) 1994-02-15
JPH0248597A (en) 1990-02-19
DK318489D0 (en) 1989-06-27
AU3712689A (en) 1990-01-04
CN1039424A (en) 1990-02-07
NO892679L (en) 1989-12-29
PT90989B (en) 1994-11-30
AU610413B2 (en) 1991-05-16
FI893162A0 (en) 1989-06-28
PT90989A (en) 1989-12-29
JP2727466B2 (en) 1998-03-11
KR900000321A (en) 1990-01-30
DE68912422D1 (en) 1994-03-03
ES2061802T3 (en) 1994-12-16
NO892679D0 (en) 1989-06-27
ZA894753B (en) 1990-03-28
PH25771A (en) 1991-10-18

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